Journal of pharmaceutical sciences最新文献_第7页

Comment on "Industry guidance on container closure integrity strategies for difficult-to-test parenteral products (DTPs)". 对“难以检测的非注射类产品（dtp）容器封闭完整性策略行业指南”的评论

IF 3.8 3区医学

Journal of pharmaceutical sciences Pub Date : 2026-05-22 DOI: 10.1016/j.xphs.2026.104340

Shweta Sharma, Talha Jawaid, Konda V V S Krishna

引用次数: 0

Evaluating hemicellulose-API miscibility using melting point depression. 用熔点下降法评价半纤维素与原料药的混相。

IF 3.8 3区医学

Journal of pharmaceutical sciences Pub Date : 2026-05-15 DOI: 10.1016/j.xphs.2026.104329

Tuomas Kilpeläinen, Riikka Laitinen

引用次数: 0

Resolving drug release mechanisms of amorphous solid dispersions using optical coherence tomography. 利用光学相干断层成像技术解决非晶固体分散体的药物释放机制。

IF 3.8 3区医学

Journal of pharmaceutical sciences Pub Date : 2026-04-29 DOI: 10.1016/j.xphs.2026.104300

Daniel Powell, Ecaterina Bordos, John Robertson, Jukka Rantanen, Daniel Markl

{"title":"Resolving drug release mechanisms of amorphous solid dispersions using optical coherence tomography.","authors":"Daniel Powell, Ecaterina Bordos, John Robertson, Jukka Rantanen, Daniel Markl","doi":"10.1016/j.xphs.2026.104300","DOIUrl":"10.1016/j.xphs.2026.104300","url":null,"abstract":"<p><p>This study presents an integrated approach utilising optical coherence tomography (OCT) to investigate the drug release mechanisms of hot-melt extruded (HME) amorphous solid dispersions (ASDs) of ritonavir and Soluplus®. Ritonavir-Soluplus® extrudates were prepared via HME using a twin-screw extruder and characterized during dissolution using a custom-designed 3D-printed flow cell, which enabled in-situ OCT imaging and continuous UV-vis monitoring of drug release. OCT provided high-resolution, time resolved visualization of structural transformations within the dissolving extrudates, while UV-vis spectroscopy quantified active pharmaceutical ingredient (API) release kinetics. Results revealed a multiphase dissolution mechanism involving sequential surface film formation, polymer swelling, delamination, and erosion. Increasing drug loading (10-30% w/w) produced marked effects on dissolution behaviour: formulations above 14% exhibited delayed release onset, extended swelling phases, and reduced overall release efficiency. OCT data showed that drug loadings above 14% led to slower erosion rates, greater swelling, and prolonged structural integrity, correlating with delayed UV-vis release profiles. Image processing using a machine learning segmentation model enabled quantitative extraction of sample cross-sectional area, confirming load-dependent swelling and erosion dynamics. Together, these findings establish a mechanistic link between structural evolution and release kinetics in HME ASDs and demonstrate the capability of OCT to provide real-time, non-destructive insight into solid dosage form dissolution. This methodology offers a powerful framework for optimizing ASD formulations and enhancing the predictive understanding of drug release mechanisms.</p>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":" ","pages":"104300"},"PeriodicalIF":3.8,"publicationDate":"2026-04-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147816602","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Sericin and alginate loaded nanocomposite hydrogels for encapsulation and oral administration of insulin 丝胶和海藻酸盐负载纳米复合水凝胶用于胰岛素包封和口服给药。

IF 3.8 3区医学

Journal of pharmaceutical sciences Pub Date : 2026-04-01 Epub Date: 2026-01-27 DOI: 10.1016/j.xphs.2026.104175

Sania Faiz, Hafiz Muhammad Tahir, Rida Mahnoor, Aamir Ali, Ayesha Muzamil, Fariha Munir, Sidra Arshad, Fatima Ijaz, Ayesha Afzal, Farwa Shafique

{"title":"Sericin and alginate loaded nanocomposite hydrogels for encapsulation and oral administration of insulin","authors":"Sania Faiz, Hafiz Muhammad Tahir, Rida Mahnoor, Aamir Ali, Ayesha Muzamil, Fariha Munir, Sidra Arshad, Fatima Ijaz, Ayesha Afzal, Farwa Shafique","doi":"10.1016/j.xphs.2026.104175","DOIUrl":"10.1016/j.xphs.2026.104175","url":null,"abstract":"<div><div>Diabetes mellitus is a major global health concern, with limited progress in the development of efficient oral insulin formulations. The current study was designed to assess the physicochemical, biochemical, and therapeutic efficiency of alginate and sericin loaded nanocomposites, which were developed as a protective oral delivery route for insulin. Ionic gelation was used to create the nanocomposites, which demonstrated excellent stability, controlled release, and high encapsulation efficiency in gastrointestinal simulations. Mice with alloxan induced diabetes were used for in-vivo evaluations. Insulin-loaded sericin-alginate nanocomposites administered orally for 21 days preserved body weight and significantly decreased fasting blood glucose levels as compared to the negative control. Blood glucose levels in the NC group increased gradually, from about 210 mg/dL to about 348 mg/dL, while 60 UI INS/60 kg reduced fasting blood glucose level from 220 mg/dL to 115 mg/dL. Significant improvements in liver and kidney function were evident by biochemical study, coupled with restored lipid profiles that showed higher HDL and lower levels of LDL, triglycerides, and cholesterol. Histological analysis revealed normal architecture of pancreatic and liver tissue in treatment groups similar to positive control. It can be concluded from the study that the sericin–alginate nanocomposites are safe, natural, and efficient oral insulin delivery method that can replace traditional subcutaneous injections.</div></div>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":"115 4","pages":"Article 104175"},"PeriodicalIF":3.8,"publicationDate":"2026-04-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146086154","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

2026 scientific advisors to the editors (SAEs) appointments and updates 2026编辑科学顾问（sae）的任命和更新。

IF 3.8 3区医学

Journal of pharmaceutical sciences Pub Date : 2026-03-01 Epub Date: 2025-12-17 DOI: 10.1016/j.xphs.2025.104131

Kenneth L. Audus

引用次数: 0

Control strategy for subvisible particulates of therapeutic protein injections in pre-filled syringes using flow imaging 利用流动成像技术对预充式注射器中治疗性蛋白注射的亚可见颗粒进行控制。

IF 3.8 3区医学

Journal of pharmaceutical sciences Pub Date : 2026-03-01 Epub Date: 2026-01-16 DOI: 10.1016/j.xphs.2026.104168

Bin Zhang , Katiria Flores , Nathyn Horvath , Nidia Gonzalez Lopez , Nishant Sawant , Eric Falcone , Stanley C. Kwok , Shalini Minocha , Vinay Radhakrishnan

{"title":"Control strategy for subvisible particulates of therapeutic protein injections in pre-filled syringes using flow imaging","authors":"Bin Zhang , Katiria Flores , Nathyn Horvath , Nidia Gonzalez Lopez , Nishant Sawant , Eric Falcone , Stanley C. Kwok , Shalini Minocha , Vinay Radhakrishnan","doi":"10.1016/j.xphs.2026.104168","DOIUrl":"10.1016/j.xphs.2026.104168","url":null,"abstract":"<div><div>Pre-filled syringes (PFSs) are a widely used container closure for therapeutic protein injections, enabling simplified preparation and at-home administration. PFSs are commonly lubricated with sprayed-on silicone oil (SiO), which may migrate into drug product as SiO particles during storage and transportation. Elevated subvisible particle (SVP) counts from SiO present challenges for meeting USP 〈788〉 specification and may raise potential immunogenicity and toxicity risks. Light Obscuration (LO), the primary compendial method for PFS product release and stability testing, cannot differentiate SiO SVPs from proteinaceous SVPs. This drives the need for more comprehensive SVP characterization approaches for PFS products. Microflow Imaging (MFI) measures SVP count, size distributions, morphology and could differentiate fibrillar and translucent proteinaceous SVPs from spherical SiO SVPs using a morphological Aspect Ratio (AR) < 0.85 filter. This manuscript proposes a SVP control strategy for PFS products using MFI, supported by data demonstrating sensitivity to particle detection and stability-indicating capability. Additional data from orthogonal FlowCam (for counts) and complementary Raman Microscopy (for SiO identification) are presented. For Protein X, MFI was tested on multiple lots and shown as effective characterization tool to develop a product-specific control strategy. The proposed SVP control strategy holds considerable promise to assess and control SVP for injectable drug products.</div></div>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":"115 3","pages":"Article 104168"},"PeriodicalIF":3.8,"publicationDate":"2026-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145998423","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Do we worry too much about polysorbate degradation? An industry-wide perspective with real-life case studies 我们是否过于担心聚山梨酯的降解？全行业视角与现实案例研究。

IF 3.8 3区医学

Journal of pharmaceutical sciences Pub Date : 2026-03-01 Epub Date: 2026-01-17 DOI: 10.1016/j.xphs.2026.104169

Klaus Wuchner , Felix Nikels , Patrick Garidel , Karoline Bechtold-Peters , Sanjay Gupta , Pierre Guibal , Linda Yi , Neil Steinmeyer , Cyrille Chery , Sebastian Peuker , Ryan E Mould , Shousong Jason Zhang , Charlie Bupp , Felix Wiggers , Yogita Krishnamachari , Indira Prajapati , Stefan Bleher

{"title":"Do we worry too much about polysorbate degradation? An industry-wide perspective with real-life case studies","authors":"Klaus Wuchner , Felix Nikels , Patrick Garidel , Karoline Bechtold-Peters , Sanjay Gupta , Pierre Guibal , Linda Yi , Neil Steinmeyer , Cyrille Chery , Sebastian Peuker , Ryan E Mould , Shousong Jason Zhang , Charlie Bupp , Felix Wiggers , Yogita Krishnamachari , Indira Prajapati , Stefan Bleher","doi":"10.1016/j.xphs.2026.104169","DOIUrl":"10.1016/j.xphs.2026.104169","url":null,"abstract":"<div><div>Polysorbates are commonly used in biotherapeutic drug formulations, but their stability over the course of the product's shelf life is a matter of concern. An industry-wide survey involving 15 biopharmaceutical companies found that 23 biotherapeutic drug products (DPs) in clinical development exhibited significant reductions in polysorbate (PS) content during long-term storage at 2–8 °C. In all cases, this decline did not impact critical quality attributes (CQAs), except for the formation of fatty acid (FA)-related sub-visible particles (SVP) in 7 DPs and FA-visible particles (VP) in 1 DP. Particle formation predominantly resulted from enzymatic or uncharacterized degradation mechanisms, not oxidative pathways. Corrective measures, such as optimization of downstream purification or reformulation, were undertaken only when SVP levels exceeded acceptable thresholds.</div><div>For PS20 and PS80, the levels of FAs generated were estimated and translated into predicted SVP levels based on theoretical assumptions. Additionally, the current understanding of PS degradation in biopharmaceuticals, based on the latest literature, is summarized, with consideration of safety and immunogenicity aspects related to the primary PS degradation products. Overall, PS degradation is considered manageable and not problematic under practical conditions. Enzymatic hydrolysis of PS is generally deemed acceptable, provided that all CQAs are maintained within specified limits. If FA-related particles are formed it is recommended that the PS degradation pathway is well characterized, and an appropriate control strategy be implemented.</div></div>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":"115 3","pages":"Article 104169"},"PeriodicalIF":3.8,"publicationDate":"2026-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146003685","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Mechanistic insights into drug loading effect on dissolution performance of Loratadine–Soluplus® amorphous solid dispersions 药物负载对氯雷他定- soluplus®非晶固体分散体溶出性能的影响机制。

IF 3.8 3区医学

Journal of pharmaceutical sciences Pub Date : 2026-03-01 Epub Date: 2026-01-30 DOI: 10.1016/j.xphs.2026.104188

Jannat Falah Hassan , Kawther Khalid Ahmed , Tze Ning Hiew

{"title":"Mechanistic insights into drug loading effect on dissolution performance of Loratadine–Soluplus® amorphous solid dispersions","authors":"Jannat Falah Hassan , Kawther Khalid Ahmed , Tze Ning Hiew","doi":"10.1016/j.xphs.2026.104188","DOIUrl":"10.1016/j.xphs.2026.104188","url":null,"abstract":"<div><div>Amorphous solid dispersions (ASDs) hold promising potential towards modulating the solubility of poorly soluble drugs. However, their use is limited by poor understanding of release mechanism and kinetics, especially with Soluplus®. In this study, we explored loratadine–Soluplus® ASDs with different drug loadings (DLs) from 3% to 15% to unveil drug content impact on dissolution, colloidal behavior, and surface composition. All formulations were fully amorphous and showed a single, composition-dependent glass transition temperature. Intrinsic dissolution testing revealed fast, nearly complete release and stable supersaturation for low-load ASDs (3–5% DL), while higher-load ASDs (10–15% DL) released more slowly, generated larger nanodroplets on liquid–liquid phase separation (LLPS), and showed precipitation upon standing. SEM imaging suggested similar surface morphology before and after partial dissolution, but EDX elemental analysis revealed congruent drug–polymer release at low DL and incongruent (polymer-first) release at high DL. These findings identify an optimum drug-loading window where ASD generates and sustains supersaturation status for loratadine, and highlight mechanistic links between DL, LLPS droplet size, and incongruent release that explain reduced performance at higher loadings.</div></div>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":"115 3","pages":"Article 104188"},"PeriodicalIF":3.8,"publicationDate":"2026-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146100353","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Quantitative prediction of human metabolites formed from the oxidation of the alcohol group of the glucokinase activator, TMG-123, using chimeric mice with humanized livers 使用人源化肝脏的嵌合小鼠，定量预测葡萄糖激酶激活剂TMG-123的醇组氧化形成的人类代谢物。

IF 3.8 3区医学

Journal of pharmaceutical sciences Pub Date : 2026-03-01 Epub Date: 2026-01-27 DOI: 10.1016/j.xphs.2026.104177

Akiko Watanabe , Seishiro Sakamoto , Shigeru Ohta , Seigo Sanoh

{"title":"Quantitative prediction of human metabolites formed from the oxidation of the alcohol group of the glucokinase activator, TMG-123, using chimeric mice with humanized livers","authors":"Akiko Watanabe , Seishiro Sakamoto , Shigeru Ohta , Seigo Sanoh","doi":"10.1016/j.xphs.2026.104177","DOIUrl":"10.1016/j.xphs.2026.104177","url":null,"abstract":"<div><div>Pharmacokinetic (PK) predictions in humans are important for both the parent compounds and their metabolites, as these predictions help decide whether to progress to human clinical trials. More human PK prediction studies have been conducted on unchanged compounds than on their metabolites. Human PK predictions are more complex for metabolites than for unchanged compounds due to the large number of metabolic enzymes involved and the need to consider species-related differences in these enzymes. Mice with humanized livers are expected to serve as simple and useful tools for assessing a wide range of metabolic enzymes. We confirmed the production of the metabolite formed from the oxidation of the alcohol group of the glucokinase activator, TMG-123, in humans; in addition, we conducted a predictive study on TMG-123 using chimeric mice. Furthermore, we identified the drug-metabolizing enzymes involved in this metabolic reaction. The in vivo production rate of GDI-1202 was 19.1% in humans, 17.0% in chimeric mice, and 5.0% in ICR mice. The main enzyme that metabolizes TMG-123 to GDI-1202 was found to be alcohol dehydrogenase (ADH)/aldehyde dehydrogenase (ALDH). Therefore, chimeric mice are effective animal models for predicting the PK of metabolites formed via the action of non-cytochrome P450 enzymes in humans.</div></div>","PeriodicalId":16741,"journal":{"name":"Journal of pharmaceutical sciences","volume":"115 3","pages":"Article 104177"},"PeriodicalIF":3.8,"publicationDate":"2026-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146086159","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

2026 scientific advisors to the editors (SAEs) appointments and updates. 2026科学顾问编辑（sae）的任命和更新。

IF 3.8 3区医学

Journal of pharmaceutical sciences Pub Date : 2026-03-01 Epub Date: 2025-12-17 DOI: 10.1016/j.xphs.2025.104131

Kenneth L Audus

引用次数: 0